N-(3-ethynylphenyl)-6,7-bis (2-methoxyethoxy)-4-quinazolinamine, in either its hydrochloride or mesylate forms, or in an anhydrous and hydrous form, is useful in the treatment of hyperproliferative disorders, such as cancers, in mammals.
U.S. Pat. No. 5,747,498, issued May 5, 1998, which is incorporated herein by reference in its entirety, refers, in Example 20, to [6,7-bis(2-methoxyethoxy)-quinazolin-4-yl]-(3-ethynylphenyl)amine hydrochloride, which, the patent discloses, is an inhibitor of the erbB family of oncogenic and protooncogenic protein tyrosine kinases, such as epidermal growth factor receptor (EGFR), and is therefore useful for the treatment of proliferative disorders, such as cancers, in humans.
The mesylate form, described in PCT International Publication No. WO 99/55683 (PCT/IB99/00612, filed Apr. 8, 1999), the entire disclosure of which is incorporated herein by reference, and assigned to a common assignee, and shown in formula 1 below:
is useful for the treatment of proliferative disorders, and more preferred with parenteral methods of administration, as compared to the hydrochloride compound, i.e. with greater effectiveness in solution.
The mesylate compounds are more soluble in aqueous compositions than the hydrochloride compound, and thus the mesylate compounds are easily delivered according to parenteral methods of administration. The hydrochloride compound is however preferred with respect to solid administration such as with tablets and oral administration.